Article

2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 1: discovery of CB2 receptor selective compounds.

Shionogi Research Laboratories, Shionogi & Co., Ltd., 12-4, Sagisu, 5-chome, Osaka 553-0002, Japan.
Bioorganic & Medicinal Chemistry Letters (impact factor: 2.55). 08/2007; 17(14):4030-4. DOI:10.1016/j.bmcl.2007.04.093 pp.4030-4
Source: PubMed

ABSTRACT 2-Arylimino-5,6-dihydro-4H-1,3-thiazines have been identified as a novel class of cannabinoid agonists. A lead structure with moderate activity was discovered through a high throughput screening assay. Structure-activity relationships led to the discovery of potent agonists of CB(2) receptor. The most potent compound 13 displays K(i) values of >5000 and 9 nM to CB(1) and CB(2) receptors, respectively.

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Keywords

moderate activity
 
novel class
 
potent agonists
 
potent compound 13 displays K(i)
 
Structure-activity relationships
 

Hiroyuki Kai